TR201810523T4 - Glukoserebrosidaz aktivatörleri olarak ornatımlı pirazolopirimidinler. - Google Patents
Glukoserebrosidaz aktivatörleri olarak ornatımlı pirazolopirimidinler. Download PDFInfo
- Publication number
- TR201810523T4 TR201810523T4 TR2018/10523T TR201810523T TR201810523T4 TR 201810523 T4 TR201810523 T4 TR 201810523T4 TR 2018/10523 T TR2018/10523 T TR 2018/10523T TR 201810523 T TR201810523 T TR 201810523T TR 201810523 T4 TR201810523 T4 TR 201810523T4
- Authority
- TR
- Turkey
- Prior art keywords
- carboxamide
- pyrimidine
- dimethylpyrazolo
- phenyl
- hydrogen
- Prior art date
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- APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 title abstract description 6
- 108010017544 Glucosylceramidase Proteins 0.000 title description 9
- 102000004547 Glucosylceramidase Human genes 0.000 title description 9
- 239000012190 activator Substances 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 88
- 239000000203 mixture Substances 0.000 claims abstract description 22
- 238000011282 treatment Methods 0.000 claims abstract description 19
- 208000015872 Gaucher disease Diseases 0.000 claims abstract description 9
- -1 cyano, nitro, amino Chemical group 0.000 claims description 38
- LPCQBTAOTIZGAE-UHFFFAOYSA-N 2h-pyrimidine-1-carboxamide Chemical compound NC(=O)N1CN=CC=C1 LPCQBTAOTIZGAE-UHFFFAOYSA-N 0.000 claims description 33
- 150000003839 salts Chemical class 0.000 claims description 29
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 27
- 125000000217 alkyl group Chemical group 0.000 claims description 25
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 239000001257 hydrogen Substances 0.000 claims description 23
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 22
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 21
- 125000001424 substituent group Chemical group 0.000 claims description 19
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 17
- 150000002367 halogens Chemical class 0.000 claims description 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 16
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 12
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 9
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 6
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- 125000004639 dihydroindenyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 5
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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| US42094610P | 2010-12-08 | 2010-12-08 |
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| TR201810523T4 true TR201810523T4 (tr) | 2018-08-27 |
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| TR2018/10523T TR201810523T4 (tr) | 2010-12-08 | 2011-12-08 | Glukoserebrosidaz aktivatörleri olarak ornatımlı pirazolopirimidinler. |
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| CN (1) | CN103534255B (es) |
| AU (1) | AU2011338377B2 (es) |
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| SI (2) | SI2649075T1 (es) |
| TR (1) | TR201810523T4 (es) |
| WO (1) | WO2012078855A1 (es) |
| ZA (1) | ZA201304215B (es) |
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| WO2012177997A1 (en) | 2011-06-22 | 2012-12-27 | The General Hospital Corporation | Treatment of proteinopathies |
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| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
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| EA201690713A1 (ru) | 2013-10-04 | 2016-08-31 | Инфинити Фармасьютикалз, Инк. | Гетероциклические соединения и их применения |
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